US4185088A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Non-adhesive ionene quaternary polymer compositions useful as bile acid sequestrants
Assignee: Merck and Co Inc
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Filing: 1978-10-19
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Granted: 1980-01-22
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Expires: 1998-10-19
Abstract
Abstract The invention disclosed herein relates to novel non-adhesive, free-flowing, pharmacologically acceptable compositions comprising ionene quaternary polymers effective as bile acid sequestrants, such as poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], adsorbed on a pulverulent, solid aggregate of large surface to mass ratio, such as fumed silicas and silica aerogels. It also relates to the novel process for preparing such adsorbate compositions which comprises forming a substantially, uniform suspension of the finely-divided solid aggregate in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing the water from the suspension, and drying the adsorbate thus produced.
Inventors
- 👤 Arthur F. Wagner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 12:05
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/74; A61K31/785; A61K9/00; A61K9/14; A61K9/141; A61K9/143
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
174 words
A bile acid sequestrant composition characterized as being non-adhesive and free-flowing after prolonged exposure to air at 35% relative humidity, which comprises a substantially uniform adsorbate of an ionene quaternary polymer on a fumed silica or silica aerogel, said polymer and silica having a weight:weight ratio of approximately 1:1, said ionene quaternary polymer having the following formula: ##STR2## wherein n is the number of repeating units in the polymer; Y is a mono- or poly-valent, pharmacologically acceptable anion, a is the anionic charge on Y, and m is the reciprocal of a; W is propyl, hydroxypropyl, allyl, alkoxypropyl, halopropyl, ammoniopropyl, alkylammoniopropyl, dialkylammoniopropyl, or trialkylammoniopropyl; Z is allyl, N-trimethylammoniopropyl-N-methyl-3-aminopropyl, N-trimethylammoniopropyl-N,N-dimethyl-3-ammoniopropyl, halopropyl, ammoniopropyl, alkylammoniopropyl, dialkylammoniopropyl or trialkylammoniopropyl; and V is the number of positively charged nitrogens (N + ) in the W and Z groupings, which is produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in an aqueous solution of said ionene quaternary polymer, evaporatively removing water from this suspension, and drying the adsorbate thus produced.
Claim 2
Dependent Claim
174 words
A bile acid sequestrant composition characterized as being non-adhesive and free-flowing after prolonged exposure to air at 35% relative humidity, which comprises a substantially uniform adsorbate of an ionene quaternary polymer on a fumed silica or silica aerogel, said polymer and silica having a weight:weight ratio of approximately 1:1, said ionene quaternary polymer having the following formula: ##STR2## wherein n is the number of repeating units in the polymer; Y is a mono- or poly-valent, pharmacologically acceptable anion, a is the anionic charge on Y, and m is the reciprocal of a; W is propyl, hydroxypropyl, allyl, alkoxypropyl, halopropyl, ammoniopropyl, alkylammoniopropyl, dialkylammoniopropyl, or trialkylammoniopropyl; Z is allyl, N-trimethylammoniopropyl-N-methyl-3-aminopropyl, N-trimethylammoniopropyl-N,N-dimethyl-3-ammoniopropyl, halopropyl, ammoniopropyl, alkylammoniopropyl, dialkylammoniopropyl or trialkylammoniopropyl; and V is the number of positively charged nitrogens (N + ) in the W and Z groupings, which is produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in an aqueous solution of said ionene quaternary polymer, evaporatively removing water from this suspension, and drying the adsorbate thus produced.
Claim 3
Dependent Claim
14 words
The bile acid sequestrant composition of claim 1, wherein said ionene is poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride}.
Claim 4
Dependent Claim
96 words
A non-adhesive, free-flowing, pharmacologically-acceptable bile acid sequestrant adsorbate composition comprising approximately equal weights of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride] and a fumed silica or silica aerogel produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in approximately 10 to 50 times its weight of water, slowly adding to this suspension, with rapid stirring, a dilute aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], and evaporating the water from the resulting suspension under reduced pressure, while stirring and maintaining the temperature of the mixture at about 25°-40° C. and drying the adsorbate thus produced.
Claim 5
Dependent Claim
96 words
A non-adhesive, free-flowing, pharmacologically-acceptable bile acid sequestrant adsorbate composition comprising approximately equal weights of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride] and a fumed silica or silica aerogel produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in approximately 10 to 50 times its weight of water, slowly adding to this suspension, with rapid stirring, a dilute aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], and evaporating the water from the resulting suspension under reduced pressure, while stirring and maintaining the temperature of the mixture at about 25°-40° C. and drying the adsorbate thus produced.
Claim 6
Dependent Claim
84 words
A unit dosage composition characterized as being non-adhesive and free-flowing after a few hours exposure to air at 35% relative humidity which comprises a tablet or capsule of about 150-300 milligrams of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride] adsorbed onto an approximately equal weight of a fumed silica or silica aerogel produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing water from this suspension, and drying the adsorbate thus produced.
Claim 7
Dependent Claim
84 words
A unit dosage composition characterized as being non-adhesive and free-flowing after a few hours exposure to air at 35% relative humidity which comprises a tablet or capsule of about 150-300 milligrams of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride] adsorbed onto an approximately equal weight of a fumed silica or silica aerogel produced by the process which comprises forming a substantially uniform suspension of a fumed silica or silica aerogel in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing water from this suspension, and drying the adsorbate thus produced.
References Cited (Backward Citations)
US4016209A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1983-01-21 | 1983-07-23 | 1984-01-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-01-21 | 1987-07-23 | 1988-01-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-01-21 | 1991-07-23 | 1992-01-22 | $7700.00 | Window Closed / Lapsed |